Bauer, Stefanie, Ochoa Puentes, Cristian, Sun, Qiu, Bause, Manuel, Bernhardt, Günther, König, Burkhard and Buschauer, Armin (2013) Quinoline carboxamide-type ABCG2 modulators: Indole and quinoline moieties as anilide replacements. ChemMedChem 8 (11), pp. 1773-1778.
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Abstract
Bioisosteric replacement of the anilide core by an indole moiety considerably increased stability and gave potent and selective ABCG2 (BCRP) inhibitors. Some compounds are superior to the reference substances fumitremorgin C and Ko143 in terms of potency and efficacy and are the most potent ABCG2 modulators reported so far.
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| Item type: | Article | ||||||
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| Date: | 28 August 2013 | ||||||
| Additional Information (public): | Umfangreiche Supporting Information (81 Seiten) | ||||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König | ||||||
| Identification Number: |
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| Keywords: | ABCB1, ABCG2, ABC transporter, breast cancer resistance protein, Inhibitors, Sonogashira coupling, Synthesis, UR COP269 | ||||||
| Dewey Decimal Classification: | 500 Science > 540 Chemistry & allied sciences 600 Technology > 615 Pharmacy | ||||||
| Status: | Published | ||||||
| Refereed: | Yes, this version has been refereed | ||||||
| Created at the University of Regensburg: | Yes | ||||||
| Item ID: | 28575 |
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